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Glossary

 Viracept® (Roche)

Approved for use in HIV infection in combination with other antiviral drugs.

DESCRIPTION: Nelfinavir inhibits the activity of HIV protease.

DOSE: Adults: 5 tablets (1250 mg) two times daily, with a meal. New formulation 625mg tablets with a slight content change may help to improve tolerability. The 625mg formulation went before the EMEA in May 2003. Paediatric: Children age 13 and younger may require (mg/kg) doses two- to three-times the adult dose to achieve similar drug concentrations. Neonates: Not determined.

SIDE EFFECTS: Diarrhoea is the most frequent side effect of nelfinavir, occurring in 20-30% of people. Over-the-counter antidiarrhoea medications such as loperamide (Imodium) usually help with nelfinavir-associated diarrhoea. Metabolic abnormalities, insulin resistance, new onset or exacerbation of diabetes mellitus and hyperglycaemia, changes in the distribution of body fat, and increased bleeding in patients with haemophilia types A and B have been reported with protease inhibitors.

TRIAL RESULTS: Nelfinavir has shown to be of value in primary infection. In antiretroviral naïve people studies showed better results with nelfinavir combined with nevirapine.

Nelfinavir/efavirenz/NRTIs - at week 40-48 – 67% had < 50 copies on ultrasensitive test.

Some studies conclude that nelfinavir may be effective after saquinavir therapy if the switch is made quickly, but that nelfinavir is not effective after failure of ritonavir or saquinavir.

At present, there are few studies on the use of nelfinavir in patients who have failed multiple protease inhibitor containing regimens.

Saquinavir/ritonavir combination or indinavir/nevirapine/plus 2 NRTIs showed viral load reductions.

RESISTANCE: There is considerable cross resistance among the PIs. Some research suggests that Nelfinavir resistant HIV may not be as virulent.

INTERACTIONS: Amprenavir: Increases nelfinavir by 15%.

Astemizole, Terfenadine, Cisapride, Midazolam, Triazolam, Rifampin must not be taken with nelfinavir.

Carbamezipine, Phenobarbital, Phenytoin: May decrease plasma levels of nelfinavir.

Didanosine: Take nelfinavir at least two hours before or one hour after didanosine.

Ethinyl Estradiol, Norethindrone: The plasma levels of these hormones may be reduced with nelfinavir.

Indinavir, Ritonavir, Saquinavir: May increase plasma levels of nelfinavir.

Rifabutin: The rifabutin dose should be reduced by half when taken with nelfinavir.

NOTE: Researchers recommend that Zocor not be prescribed with nelfinavir and that Lipitor and nelfinavir be used with caution.

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